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Laetrile/Amygdalin (PDQ®)

History

Amygdalin was first isolated in 1830 by two French chemists.[1,2] It was used as an anticancer agent in Russia as early as 1845, and
positive results were reported for the first patient treated.[3,4] The first recorded use of amygdalin in the United States as a treatment for cancer occurred in
the early 1920s.[5] At that time, amygdalin was taken in pill
form; however, the formulation was judged too toxic, and the work was
abandoned. In the 1950s, a purportedly nontoxicintravenous form of amygdalin
was patented as Laetrile.[1,6,7]

Laetrile has been tested on cultured animal cells (cells grown
in specialized containers in the laboratory), in whole animals, in xenograft models (tumor cells from one
species transplanted onto another species), and in humans to determine whether
it has specific anticancer properties (an ability to kill cancer cells more
readily than normal cells). As noted previously (General Information), cyanide is believed to be the main cancer-killing ingredient in
laetrile.[8,9] When amygdalin interacts with the enzyme beta-glucosidase
or undergoes hydrolysis (breakdown in
a reaction with water) in the absence of enzymes, hydrogen cyanide, benzaldehyde, and glucose (sugar) are
produced.[1,7,8,10,11] Cyanide can also be produced from
prunasin, which is a less-than-complete breakdown product of
amygdalin.[1,8]

Four different theories have been advanced to explain the anticancer
activity of laetrile. The first of these incorporates elements of the
trophoblastic theory of cancer, a theory that is not widely accepted as an
explanation for cancer formation. According to the trophoblastic theory, all
cancers arise from primordial germ cells (cells that, under normal
circumstances, would give rise to eggs or sperm), some of which become
dispersed throughout the body during embryonic development and, therefore, are not confined to the testes or ovaries. The trophoblastic theory also suggests that transformation of
primordial germ cells to a cancerous state is normally prevented by enzymes
from the pancreas, and that cancers can
be destroyed by pancreatic enzyme supplements and treatment with laetrile.[12-17] The rationale
for laetrile use is the suggestion that malignant cells have higher than
normal levels of an enzyme called beta-glucuronidase (which is different from
the aforementioned enzyme beta-glucosidase) and that they are deficient in
another enzyme called rhodanese (thiosulfate sulfurtransferase).Another suggestion is that laetrile is modified in the liver, and that
beta-glucuronidase breaks down the modified compound, ultimately producing
cyanide. Rhodanese can convert cyanide into the relatively harmless compound
thiocyanate. Thus, it has been proposed that cancer cells are more
susceptible to the toxic effects of laetrile than normal cells because of an
imbalance in these two enzymes.[10,13,18-20] Some experimental evidence does support the idea that normal tissues and malignant tissues differ substantially in their concentrations of
beta-glucuronidase [21] and rhodanese.[22,23]

The second theory states that cancer cells contain more beta-glucosidase
activity than normal cells and, as in the first theory, that they are
deficient in rhodanese.[1,5,13,15,18,24,25] Again, elevated beta-glucosidase activity in the interstitial regions of some malignancies has been experimentally demonstrated.[26,27]

The third theory states that cancer is the result of a metabolic disorder caused by a vitamindeficiency. It states further that laetrile, or “vitamin B-17,” is
the missing vitamin needed by the body to restore health.[18,28-30] Experimental evidence indicates that the level of intake of
individual vitamins and/or the vitamin status of an organism can influence the development of
cancer, but there is no evidence that laetrile is needed for normal metabolism or that it can function as a
vitamin in animals or humans.[31,32]

The fourth theory suggests that the cyanide released by laetrile has a
toxic effect beyond its interference with oxygen utilization by cells.
According to this theory, cyanide increases the acid content of tumors and
leads to the destruction of lysosomes (compartments inside cells that contain enzymes capable of breaking down other
cellular molecules). The injured
lysosomes release their contents, thereby killing the cancer cells and
arresting tumor growth.[15] According to this theory, another
consequence of lysosome disruption is stimulation of the immune system.